Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein X, R1, R2, R3, R4, and m are defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.
Abstract: N-oxide pyrazine derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: R1. R2, R3, R4, and R5 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.
Abstract: The amide compound of the formula (I) [each symbol is as defined in the description] has a promoting action on neuritogenesis of trigeminal nerve cells, and the compound is useful as a corneal neuritogenesis promoter, an agent for recovering corneal sensitivity by promotion of corneal neuritogenesis, and an agent for treating dry eye.
Abstract: The invention provides a salt of (R)-3-[2-(2-hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one and a crystal thereof. (R)-3-[2-(2-Hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one monophosphate is a compound which is chemically stable, has high solubility, and shows less weight change due to humidity as compared to a free form and monohydrochloride dihydrate, and is superior as a bulk drug for pharmaceutical products.
Abstract: A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); a pharmaceutically acceptable salt thereof, or a prodrug thereof.
Abstract: A novel crystal form of 1-(?-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and/or by its infra-red spectrum.
Abstract: Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is halogen, or alkyl, R2 is hydrogen, or halogen, Ar is phenyl, or thienyl, which may be substituted with halogen, alkyl, alkoxy, alkylthio, etc.
Abstract: A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is hydrogen atom and the like or a pharmaceutically acceptable salt thereof, and a hydrate or solvate thereof have affinity for CCR3, and can be pharmaceutical products for the treatment and/or prophylaxis of immune or inflammatory diseases.
Abstract: Intraorally rapidly disintegrating tablets which, when ingested, disintegrates in the oral cavity rapidly without presenting unpleasant taste, can be quickly absorbed in the digestive tract and express efficacy are provided. The intraorally rapidly disintegrating tablets contain a drug being hardly water-soluble under neutral or alkaline conditions and being highly water-soluble under acidic conditions yet presenting unpleasant taste, which tablets can be prepared by combining the medicinal substance with a water-soluble acidic substance, coating either or both of the substances with a water-soluble coating agent being insoluble in alcoholic solvent, further adding a water-soluble binding agent being soluble in alcoholic solvent and a water-soluble saccharide, subjecting the resultant mixture to compression, and treating the products with an alcoholic solvent.
Abstract: A therapeutic drug for cancer containing a substance selected from the group consisting of a novel cyanopyridine derivative, a pharmaceutically acceptable salt, a hydrate, a water adduct and a solvate as an active ingredient can be provided.
Abstract: The present invention provides and a plastic container and multilayered films, which comprises a heat-sealable seal layer, a cyclic polyolefin layer, and an outermost layer, wherein the seal layer comprises polypropylene, the cyclic polyolefin layer comprises a cyclic polyolefin polymer or a cyclic polyolefin copolymer, and the outermost layer comprises a layer containing polypropylene, and which further comprises a resin composition layer comprises a blended product of a propylene polymer and a styrene elastomer. The plastic container of the present invention can suppresses a reduction in the medicament content of a liquid-state medicament and is excellent in terms of shock resistance, handling ability during the filling of the container with the medicament, and the moldability and transparency of the container.
Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
Abstract: The present invention aims at providing a pharmaceutical composition for the prophylaxis or treatment, irrespective of the kind of virus, of viral myocarditis or viral diseases induced by viral myocarditis, by the treatment or prevention of the onset of cytotoxicity in various organs, and a method of the prophylaxis or treatment. The present invention also relates to a pharmaceutical composition for the prophylaxis or treatment of viral myocarditis or viral diseases induced by viral myocarditis, which contains 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3-diol or a pharmacologically acceptable salt thereof as an active ingredient. The present invention further relates to a method for the prophylaxis or treatment of viral myocarditis or viral diseases induced by viral myocarditis, which includes administering an effective amount of the aforementioned compound or a pharmacologically acceptable salt thereof.
Abstract: A novel preventive and/or therapeutic medicament for a constipation predominant IBS which contains as the active ingredient a thieno[3,2-b]pyridinecarboxamide derivative represented by the formula (I): wherein R1 and R2 each independently represents hydrogen atom or a lower alkyl group and A represents a substituent selected from the group consisting of 1-azabicyclo[3.2.2]nonyl group 1-azabicyclo[2.2.2]octyl group, and the N-oxides thereof, a pharmaceutically acceptable salt thereof, or a solvate or hydrate thereof.
Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.
Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.
Abstract: It is mentioned to provide drugs for ameliorating postcibal hyperglycemia, drugs for inhibiting an increase in blood glucose level and pharmaceutical compositions for preventing or treating diabetes, each containing a pharmaceutically acceptable anion exchange resin typified by colestimide. Thus, it becomes possible to provide drugs clearly exhibiting an effect of inhibiting an increase in postcibal blood glucose level.
Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
Abstract: The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y, Z, R1, R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.